Imidazoacridinones arrest cell-cycle progression in the G2 phase of L1210 cells

Cancer Chemotherapy and Pharmacology
Ewa AugustinJ Konopa

Abstract

Imidazoacridinones are a new class of highly potent antineoplastic agents synthesised at the Technical University of Gdansk. The pharmacophoric alkyldiamine group, which is also present in anthracenediones (e.g. ametantrone, mitoxantrone), has been shown to be responsible for their antineoplastic activity. In view of their chemical similarity to anthracenediones, we anticipated that the imidazoacridinones would have a mechanism of action similar to that of these agents and that this would be reflected by a similar influence on cell-cycle progression. Flow cytometry was used to monitor the effect of three derivatives of imidazoacridinone (C-1263, C-1310 and C-1311) on L1210 cell cycle traverse at concentrations ranging from 0.01 to 0.9 microgram/ml, corresponding to their 50% and 90% effective concentrations (EC50 and EC90 values), over times of drug treatment ranging from 1 to 48 h. The results demonstrate that all of the compounds produced a similar effect, inducing preferential and complete arrest (accumulation) of cells in the G2 phase of the cell cycle (i.e. G2 block). The kinetics of the induction of G2 arrest were dependent on both the dose and the duration of treatment. Cell-cycle arrest was reversible for up to about 3 ...Continue Reading

Citations

Oct 10, 2007·Apoptosis : an International Journal on Programmed Cell Death·Anna SkwarskaJerzy Konopa
May 15, 2002·Biochemical Pharmacology·Jaroslaw DziegielewskiJerzy Konopa
Sep 29, 2001·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·N ZaffaroniJ A Double
Dec 25, 2009·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·N IsambertP Fumoleau
Feb 16, 2005·Biochemical Pharmacology·Magdalena HyzyAndrzej Skladanowski
May 8, 2015·Cell Death & Disease·S MahaleB Chaudhuri
Feb 8, 2006·Journal of Oncology Pharmacy Practice : Official Publication of the International Society of Oncology Pharmacy Practitioners·Monique W J den BrokJos H Beijnen
May 11, 2011·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Agnieszka PotegaZofia Mazerska
Oct 19, 2007·Journal of Biomolecular Screening·Juergen FriedrichLeoni A Kunz-Schughart

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